Invention Grant
- Patent Title: Methanesulfonate polymorph of 5-type phosphodiesterase inhibitor and preparation method and applications thereof
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Application No.: US16317208Application Date: 2017-07-26
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Publication No.: US10654859B2Publication Date: 2020-05-19
- Inventor: Jinglin Wang , Ruimei Yu , Qiongqiong Lian
- Applicant: JINAN MEILUWEI BIOTECHNOLOGY CO., LTD.
- Applicant Address: CN Shandong
- Assignee: JINAN MEILUWEI BIOTECHNOLOGY CO., LTD.
- Current Assignee: JINAN MEILUWEI BIOTECHNOLOGY CO., LTD.
- Current Assignee Address: CN Shandong
- Agency: Oliff PLC
- Priority: com.zzzhc.datahub.patent.etl.us.BibliographicData$PriorityClaim@298a2c80
- International Application: PCT/CN2017/094467 WO 20170726
- International Announcement: WO2018/209809 WO 20181122
- Main IPC: C07D487/04
- IPC: C07D487/04

Abstract:
A methanesulfonate polymorph of a 5-type phosphodiesterase inhibitor. The structure of the 5-type phosphodiesterase inhibitor is as shown in formula A: The methanesulfonate polymorph of the 5-type phosphodiesterase inhibitor includes the following diffraction peaks measured at 2θ reflection angles in an X-ray powder diffraction pattern: 7.1750°±0.2°, 7.6299°±0.2°, 8.8588°±0.2°, 13.2310°±0.2°, 14.3754°±0.2°, 14.8440±0.2°, 15.2941°±0.2°, 17.1838°±0.2°, 20.0314°±0.2°, 20.8507°±0.2°, 21.2839°±0.2°, 21.7890°±0.2°, 22.2594°±0.2°, 23.0373±0.2°, 25.1243°±0.2°, 25.4244°±0.2°, 26.1530°±0.2°, 28.1210°±0.2°, 30.0135°±0.2°, 31.4809°±0.2°, 32.3619°±0.2°, 37.2410°±0.2°, 37.6388°±0.2° and 40.8286°±0.2°. The methanesulfonate of the 5-type phosphodiesterase inhibitor not only improves the activity of drugs, but also improves the water solubility and the bioavailability of the drugs, and makes up the blank of studies on drugs of the crystal form.
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